BMY-7378 IS A SELECTIVE ANTAGONIST OF THE D-SUBTYPE OF ALPHA(1)-ADRENOCEPTORS

Citation
As. Goetz et al., BMY-7378 IS A SELECTIVE ANTAGONIST OF THE D-SUBTYPE OF ALPHA(1)-ADRENOCEPTORS, European journal of pharmacology, 272(2-3), 1995, pp. 5-6
Citations number
8
Categorie Soggetti
Pharmacology & Pharmacy
ISSN journal
00142999
Volume
272
Issue
2-3
Year of publication
1995
Pages
5 - 6
Database
ISI
SICI code
0014-2999(1995)272:2-3<5:BIASAO>2.0.ZU;2-B
Abstract
BMY 7378 piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione dihydrochl oride), a 5-HT1A receptor partial agonist, also binds to alpha(1)-adre noceptors. Competition assays were performed using ]ioda-4-hydroxyphen yl)-ethyl-aminomethyl-tetralone ([I-125]HEAT), membranes prepared from Rat-1 fibroblasts expressing hamster alpha(1b)-, bovine (alpha(1c)-, or rat alpha(1d)-adrenoceptor, or their respective human homologues. R esults indicate that BMY 7378 is selective for the alpha(1D)-adrenocep tor subtype (pK(i): hamster alpha(1b)-adrenoceptor 6.2 +/- 0.03, human alpha(1b)-adrenoceptor 7.2 +/- 0.05; bovine alpha(1c)-adrenoceptor 6. 1 +/- 0.02, human alpha(1c)-adrenoceptor 6.6 +/- 0.20; rat alpha(1d)-a drenoceptor 8.2 +/- 0.06, human alpha(1d)-adrenoceptor 9.4 +/- 0.05) a nd has high affinity (pA(2), 8.9 +/- 0.1) for rat aorta alpha(1)-adren oceptor.